Peringatan Keamanan

There is no difference in effect across gendersA177184,Label. The difference in effect across racial groups, patients under 6 years, renal impairment, hepatic impairment, pregnancy, lactation, and geriatric patients has not been well studied. Patients with renal impairment are not expected to need dose adjustment as the drug is not mainly cleared renallyLabel. Animal studies in pregnant and lactating rats showed delayed fetal skeletal ossification, and reduced weight gain in male offspringLabel. Due to these studies, caution must be exercised and the benefits and risks of taking this drug must be weighedLabel. It is unlikely that dexmethylphenidate is carcinogenic but B6C3F1 mice, which are sensitive to the development of hepatic tumours, developed hepatoblastomas at 2 times the maximum recommended human doseLabel. Methylpheidate was not found to be mutagenic but is weakly clastogenic in Chinese Hamster Ovary cellsLabel. Methylphenidate does not impair fertility in animal studiesLabel.

Dexmethylphenidate

DB06701

small molecule approved investigational

Deskripsi

Dexmethylphenidate is the dextrorotary form of methylphenidate introduced in 2002A177181. It is a norepinephrine-dopamine reuptake inhibitor (NDRI) and thus a psychostimulantA177193. It is used for treatment of Attention Deficit Hyperactivity Disorder (ADHD)Label,A177181. The d-isomer is thought to have greater effect with fewer side effects than the l-isomer or the racemic mixtureA177181.

Struktur Molekul 2D

Berat 233.3062
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean terminal half life is approximately 2.2 hours[Label]. However other studies have shown 3.8-3.9 hours[A177184], or 5.96 hours after intravenous administration and 5.69 hours following an oral dose[A177187].
Volume Distribusi 2.65L/kg when administered intravenously[A177187].
Klirens (Clearance) 0.40L/hr/kg following an intravenous dose and a renal clearance of 0.005L/hr/kg[A177187,Label].

Absorpsi

Taking dexmethylphenidate with or without food does not affect patients in a clinically relevant wayA177187. 90% of an oral dose is absorbedLabel but as a result of hepatic first pass metabolism, oral bioavailability of dexmethylphenidate is 23% compared to l-methylphenidate with an oral bioavailability of 5% A177187. Maximum concentration is generally reached in 1-1.5 hoursLabel.

Metabolisme

Dexmethylphenidate is metabolised to the inactive metabolite ritalinic acid by carboxylesterase 1A1 in the liverLabel,A176038. Other minor pathways metabolise dexmethylphenidate to the inactive metabolites 6-oxo-methylphenidate and p-hydroxy-methylphenidate which are de-esterified and conjugated into other unknown metabolitesA177187.

Rute Eliminasi

Dexmethylphenidate is mainly eliminated renallyA177187. After 48 hours, 90% of the dose is collected in the urine and 3.3% is collected from fecesA177187.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Alcohol inhibits the metabolism of dexmethylphenidate.
  • 2. Take with or without food.

Interaksi Obat

1152 Data
Valsartan Dexmethylphenidate may decrease the antihypertensive activities of Valsartan.
Ramipril Dexmethylphenidate may decrease the antihypertensive activities of Ramipril.
Esmolol Dexmethylphenidate may decrease the antihypertensive activities of Esmolol.
Betaxolol Dexmethylphenidate may decrease the antihypertensive activities of Betaxolol.
Reserpine Dexmethylphenidate may decrease the antihypertensive activities of Reserpine.
Remikiren Dexmethylphenidate may decrease the antihypertensive activities of Remikiren.
Torasemide Dexmethylphenidate may decrease the antihypertensive activities of Torasemide.
Bethanidine Dexmethylphenidate may decrease the antihypertensive activities of Bethanidine.
Guanadrel Dexmethylphenidate may decrease the antihypertensive activities of Guanadrel.
Metoprolol Dexmethylphenidate may decrease the antihypertensive activities of Metoprolol.
Isradipine Dexmethylphenidate may decrease the antihypertensive activities of Isradipine.
Olmesartan Dexmethylphenidate may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Dexmethylphenidate may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Dexmethylphenidate may decrease the antihypertensive activities of Nitroprusside.
Atenolol Dexmethylphenidate may decrease the antihypertensive activities of Atenolol.
Diltiazem Dexmethylphenidate may decrease the antihypertensive activities of Diltiazem.
Minoxidil Dexmethylphenidate may decrease the antihypertensive activities of Minoxidil.
Timolol Dexmethylphenidate may decrease the antihypertensive activities of Timolol.
Treprostinil Dexmethylphenidate may decrease the antihypertensive activities of Treprostinil.
Amlodipine Dexmethylphenidate may decrease the antihypertensive activities of Amlodipine.
Nimodipine Dexmethylphenidate may decrease the antihypertensive activities of Nimodipine.
Nisoldipine Dexmethylphenidate may decrease the antihypertensive activities of Nisoldipine.
Bendroflumethiazide Dexmethylphenidate may decrease the antihypertensive activities of Bendroflumethiazide.
Prazosin Dexmethylphenidate may decrease the antihypertensive activities of Prazosin.
Fosinopril Dexmethylphenidate may decrease the antihypertensive activities of Fosinopril.
Trandolapril Dexmethylphenidate may decrease the antihypertensive activities of Trandolapril.
Metolazone Dexmethylphenidate may decrease the antihypertensive activities of Metolazone.
Lercanidipine Dexmethylphenidate may decrease the antihypertensive activities of Lercanidipine.
Benazepril Dexmethylphenidate may decrease the antihypertensive activities of Benazepril.
Bosentan Dexmethylphenidate may decrease the antihypertensive activities of Bosentan.
Propranolol Dexmethylphenidate may decrease the antihypertensive activities of Propranolol.
Enalapril Dexmethylphenidate may decrease the antihypertensive activities of Enalapril.
Doxazosin Dexmethylphenidate may decrease the antihypertensive activities of Doxazosin.
Labetalol Dexmethylphenidate may decrease the antihypertensive activities of Labetalol.
Cyclothiazide Dexmethylphenidate may decrease the antihypertensive activities of Cyclothiazide.
Bisoprolol Dexmethylphenidate may decrease the antihypertensive activities of Bisoprolol.
Candoxatril Dexmethylphenidate may decrease the antihypertensive activities of Candoxatril.
Nicardipine Dexmethylphenidate may decrease the antihypertensive activities of Nicardipine.
Guanabenz Dexmethylphenidate may decrease the antihypertensive activities of Guanabenz.
Mecamylamine Dexmethylphenidate may decrease the antihypertensive activities of Mecamylamine.
Losartan Dexmethylphenidate may decrease the antihypertensive activities of Losartan.
Moexipril Dexmethylphenidate may decrease the antihypertensive activities of Moexipril.
Phentolamine Dexmethylphenidate may decrease the antihypertensive activities of Phentolamine.
Eplerenone Dexmethylphenidate may decrease the antihypertensive activities of Eplerenone.
Lisinopril Dexmethylphenidate may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Dexmethylphenidate may decrease the antihypertensive activities of Nitroglycerin.
Hydroflumethiazide Dexmethylphenidate may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Dexmethylphenidate may decrease the antihypertensive activities of Cryptenamine.
Perindopril Dexmethylphenidate may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Dexmethylphenidate may decrease the antihypertensive activities of Candesartan cilexetil.
Tolazoline Dexmethylphenidate may decrease the antihypertensive activities of Tolazoline.
Fenoldopam Dexmethylphenidate may decrease the antihypertensive activities of Fenoldopam.
Indapamide Dexmethylphenidate may decrease the antihypertensive activities of Indapamide.
Tadalafil Dexmethylphenidate may decrease the antihypertensive activities of Tadalafil.
Alprenolol Dexmethylphenidate may decrease the antihypertensive activities of Alprenolol.
Eprosartan Dexmethylphenidate may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Dexmethylphenidate may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Dexmethylphenidate may decrease the antihypertensive activities of Quinapril.
Omapatrilat Dexmethylphenidate may decrease the antihypertensive activities of Omapatrilat.
Phenoxybenzamine Dexmethylphenidate may decrease the antihypertensive activities of Phenoxybenzamine.
Pindolol Dexmethylphenidate may decrease the antihypertensive activities of Pindolol.
Telmisartan Dexmethylphenidate may decrease the antihypertensive activities of Telmisartan.
Methyldopa Dexmethylphenidate may decrease the antihypertensive activities of Methyldopa.
Hydrochlorothiazide Dexmethylphenidate may decrease the antihypertensive activities of Hydrochlorothiazide.
Guanfacine Dexmethylphenidate may decrease the antihypertensive activities of Guanfacine.
Trichlormethiazide Dexmethylphenidate may decrease the antihypertensive activities of Trichlormethiazide.
Felodipine Dexmethylphenidate may decrease the antihypertensive activities of Felodipine.
Irbesartan Dexmethylphenidate may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Dexmethylphenidate may decrease the antihypertensive activities of Nitrendipine.
Deserpidine Dexmethylphenidate may decrease the antihypertensive activities of Deserpidine.
Pentolinium Dexmethylphenidate may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Dexmethylphenidate may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Dexmethylphenidate may decrease the antihypertensive activities of Diazoxide.
Carvedilol Dexmethylphenidate may decrease the antihypertensive activities of Carvedilol.
Bretylium Dexmethylphenidate may decrease the antihypertensive activities of Bretylium.
Terazosin Dexmethylphenidate may decrease the antihypertensive activities of Terazosin.
Guanethidine Dexmethylphenidate may decrease the antihypertensive activities of Guanethidine.
Rescinnamine Dexmethylphenidate may decrease the antihypertensive activities of Rescinnamine.
Acebutolol Dexmethylphenidate may decrease the antihypertensive activities of Acebutolol.
Captopril Dexmethylphenidate may decrease the antihypertensive activities of Captopril.
Nadolol Dexmethylphenidate may decrease the antihypertensive activities of Nadolol.
Epoprostenol Dexmethylphenidate may decrease the antihypertensive activities of Epoprostenol.
Bepridil Dexmethylphenidate may decrease the antihypertensive activities of Bepridil.
Hydralazine Dexmethylphenidate may decrease the antihypertensive activities of Hydralazine.
Bevantolol Dexmethylphenidate may decrease the antihypertensive activities of Bevantolol.
Practolol Dexmethylphenidate may decrease the antihypertensive activities of Practolol.
Polythiazide Dexmethylphenidate may decrease the antihypertensive activities of Polythiazide.
Cilazapril Dexmethylphenidate may decrease the antihypertensive activities of Cilazapril.
Saprisartan Dexmethylphenidate may decrease the antihypertensive activities of Saprisartan.
Spirapril Dexmethylphenidate may decrease the antihypertensive activities of Spirapril.
Penbutolol Dexmethylphenidate may decrease the antihypertensive activities of Penbutolol.
Mibefradil Dexmethylphenidate may decrease the antihypertensive activities of Mibefradil.
Oxprenolol Dexmethylphenidate may decrease the antihypertensive activities of Oxprenolol.
Dexpropranolol Dexmethylphenidate may decrease the antihypertensive activities of Dexpropranolol.
Tienilic acid Dexmethylphenidate may decrease the antihypertensive activities of Tienilic acid.
Debrisoquine Dexmethylphenidate may decrease the antihypertensive activities of Debrisoquine.
Celiprolol Dexmethylphenidate may decrease the antihypertensive activities of Celiprolol.
Nebivolol Dexmethylphenidate may decrease the antihypertensive activities of Nebivolol.
Sitaxentan Dexmethylphenidate may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Dexmethylphenidate may decrease the antihypertensive activities of Ambrisentan.

Target Protein

Sodium-dependent dopamine transporter SLC6A3
Sodium-dependent noradrenaline transporter SLC6A2
Sodium-dependent serotonin transporter SLC6A4

Referensi & Sumber

Synthesis reference: Arie Gutman, "Process for the preparation of dexmethylphenidate hydrochloride." U.S. Patent US20040180928, issued September 16, 2004.
Artikel (PubMed)
  • PMID: 15082749
    Sun Z, Murry DJ, Sanghani SP, Davis WI, Kedishvili NY, Zou Q, Hurley TD, Bosron WF: Methylphenidate is stereoselectively hydrolyzed by human carboxylesterase CES1A1. J Pharmacol Exp Ther. 2004 Aug;310(2):469-76. doi: 10.1124/jpet.104.067116. Epub 2004 Apr 13.
  • PMID: 19412495
    Liu F, Minami H, Silva RR: Dexmethylphenidate hydrochloride in the treatment of attention deficit hyperactivity disorder. Neuropsychiatr Dis Treat. 2006 Dec;2(4):467-73.
  • PMID: 11028253
    Modi NB, Wang B, Noveck RJ, Gupta SK: Dose-proportional and stereospecific pharmacokinetics of methylphenidate delivered using an osmotic, controlled-release oral delivery system. J Clin Pharmacol. 2000 Oct;40(10):1141-9.
  • PMID: 10628897
    Kimko HC, Cross JT, Abernethy DR: Pharmacokinetics and clinical effectiveness of methylphenidate. Clin Pharmacokinet. 1999 Dec;37(6):457-70. doi: 10.2165/00003088-199937060-00002.
  • PMID: 30847388
    Tremblay S, Pieper F, Sachs A, Joober R, Martinez-Trujillo J: The Effects of Methylphenidate (Ritalin) on the Neurophysiology of the Monkey Caudal Prefrontal Cortex. eNeuro. 2019 Mar 4;6(1). pii: eN-NWR-0371-18. doi: 10.1523/ENEURO.0371-18.2018. eCollection 2019 Jan-Feb.

Contoh Produk & Brand

Produk: 209 • International brands: 1
Produk
  • Attenade
    Tablet • 2.5 mg • Oral • Canada • Approved
  • Attenade
    Tablet • 5 mg • Oral • Canada • Approved
  • Attenade
    Tablet • 10 mg • Oral • Canada • Approved
  • Azstarys
    Capsule • - • Oral • US • Approved
  • Azstarys
    Capsule • - • Oral • US • Approved
  • Azstarys
    Capsule • - • Oral • US • Approved
  • Dexmethylphenidate HCl
    Capsule • 5 mg/1 • Oral • US • Generic • Approved
  • Dexmethylphenidate HCl
    Capsule • 10 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 209 produk.
International Brands
  • Attenade — Celgene

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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